Introduction：Basic information about CAS 1362850-20-1|Seletalisib, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Seletalisib |
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| CAS Number | 1362850-20-1 | Molecular Weight | 482.845 |
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| Density | 1.5±0.1 g/cm3 | Boiling Point | 710.8±60.0 °C at 760 mmHg |
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| Molecular Formula | C23H14ClF3N6O | Melting Point | / |
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| MSDS | / | Flash Point | 383.7±32.9 °C |
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Names
| Name | Seletalisib |
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| Synonym | More Synonyms |
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Seletalisib BiologicalActivity
| Description | Seletalisib (UCB5857) is potent and selective PI3Kδ inhibitor with an IC50 of 12 nM. |
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| Related Catalog | Research Areas >>Inflammation/Immunology |
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| Target | PI3Kδ:12 nM (IC50) |
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| In Vitro | Seletalisib is a potent, ATP-competitive and highly selective PI3Kδ inhibitor able to block AKT phosphorylation following activation of the BCR in a B-cell line. Seletalisib inhibits N-formyl peptides (fMLP)-stimulated but not phorbol myristate acetate (PMA)-stimulated superoxide release from human neutrophils consistent with a PI3Kδ-specific activity. No indications of cytotoxicity are observed in PBMCs or other cell types treated with seletalisib. seletalisib blocks human T-cell production of several cytokines from activated T-cells. Seletalisib inhibits T-cell differentiation to Th1, Th2, and Th17 subtypes. Additionally, seletalisib inhibits B-cell proliferation and cytokine release. In human whole blood assays, seletalisib inhibits CD69 expression upon B-cell activation and anti-IgE-mediated basophil degranulation[1]. |
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| In Vivo | Seletalisib significantly inhibits IL-2 release following TCR stimulation in the rat. The inhibition is observed at all tested doses of seletalisib with almost complete inhibition reached at dose levels ≥1 mg/kg. Seletalisib has potent in vivo effects with an estimated IC50 value of <10 nM[1]. |
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| Kinase Assay | Seletalisib is dissolved 1 mM solution in DMSO, and tested in a concentration response (seletalisib), to explore the effects of PI3Kδ-specific inhibition compared with complete inhibition of class I PI3K signaling. In addition, seletalisib is tested in the BioMap BT cell system at concentrations of 1000, 100, 10, and 1 nM. An activity profile is generated based on the effect of the compounds on the levels of cellular readouts, including cytokines, growth factors, adhesion molecules, and proliferation endpoints[1]. |
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| Animal Admin | Rats: Rats are dosed with seletalisib (0.1-10 mg/kg in 500 μL volume) or vehicle via oral gavage 30 min prior to i.v. administration of anti- CD3 antibody administered in a 200 μL dose volume. The vehicle is methylcellulose or saline for oral and i.v. administration, respectively. Seletalisib levels and IL-2 levels are measured[1]. |
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| References | [1]. Allen RA, et al. Seletalisib: Characterization of a Novel, Potent, and Selective Inhibitor of PI3Kδ. J Pharmacol Exp Ther. 2017 Apr 25. pii: jpet.116.237347. |
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Chemical & Physical Properties
| Density | 1.5±0.1 g/cm3 |
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| Boiling Point | 710.8±60.0 °C at 760 mmHg |
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| Molecular Formula | C23H14ClF3N6O |
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| Molecular Weight | 482.845 |
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| Flash Point | 383.7±32.9 °C |
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| Exact Mass | 482.086975 |
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| LogP | 2.21 |
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| Vapour Pressure | 0.0±2.3 mmHg at 25°C |
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| Index of Refraction | 1.692 |
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| Storage condition | -20℃ |
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Synonyms
| Seletalisib |
| UNII-64CW205BDD |
| 64CW205BDD |
| N-{(1R)-1-[8-Chloro-2-(1-oxido-3-pyridinyl)-3-quinolinyl]-2,2,2-trifluoroethyl}pyrido[3,2-d]pyrimidin-4-amine |
| Pyrido[3,2-d]pyrimidin-4-amine, N-[(1R)-1-[8-chloro-2-(1-oxido-3-pyridinyl)-3-quinolinyl]-2,2,2-trifluoroethyl]- |
